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  • Endocrinology-Hormones

Endocrinology-Hormones

Small molecules play a pivotal role in Endocrinology Research. These are low molecular weight compounds that have a significant impact on the endocrine system, hormones, and their receptors. Here are some key aspects of how small molecules are involved in this field:

  • Hormone Mimetics and Inhibitors: Small molecules are used to develop synthetic compounds that mimic the actions of hormones or inhibit their effects. For example, drugs like metformin for diabetes management and selective estrogen receptor modulators (SERMs) for breast cancer treatment are used to either mimic or block hormonal activity.
  • Receptor Modulation: Small molecules can bind to hormone receptors and modulate their activity. This is crucial in developing drugs that target specific hormone receptors, like the use of small molecule agonists and antagonists to regulate thyroid hormone receptors.
  • Metabolism Regulation: Endocrinology research often focuses on metabolism and how hormones like insulin regulate it. Small molecules are employed to understand and develop drugs targeting enzymes involved in metabolism, such as glucagon-like peptide-1 (GLP-1) agonists for diabetes treatment.
  • Steroid Hormone Production: Small molecules may be utilized to influence the production of steroid hormones in the adrenal glands or gonads. This is essential for conditions like Cushing's syndrome or polycystic ovary syndrome (PCOS).
  • Hormone Assays: In laboratory research, small molecules are used as tracers or markers in hormone assays. For instance, small molecule fluorophores can be attached to antibodies to detect hormone levels in blood samples.

Drug Development: Endocrinology research relies on small molecules as potential drug candidates. Researchers design and test small molecules for their effectiveness in modulating hormonal pathways, with the goal of developing new therapies for endocrine disorders.
In summary, small molecules are indispensable tools in Endocrinology Research, enabling scientists to better understand the endocrine system's intricacies and develop novel treatments for a wide range of hormonal disorders and conditions. Their versatility and specificity make them valuable assets in advancing our knowledge of endocrinology and improving patient care.

Endocrinology Disease Products

Diabetes Research

Endocrinology Research Products

Kisspeptin Receptor

Leptin Receptors

Melanocortin (MC) Receptors

Mineralocorticoid Receptors

Galanin Receptors

TRH Receptors

Ghrelin Receptors

Natriuretic Peptide Receptors

NPY Receptors

Motilin Receptor

PTH Receptor

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Items 1-50 of 125

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Citations
  1. A10495
    Kaempferol

    ERRα and ERRγ inverse agonist

    Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.
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  2. A16986
    (R)-Equol

    Estrogen receptor agonist

    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
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  3. A10439
    GSK1292263

    GPR119 agonist

    GSK-1292263 is a novel GPR119 agonist.
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  4. A12376
    SR 144528

    CB2 inverse agonist

    SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.
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  5. A16956
    GSK4716

    ERRβ & ERRγ Agonist

    GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ
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  6. A19383
    GSK5182

    ERRγ agonist

    GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.
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  7. A10299
    Dexamethasone

    glucocorticoid receptor agonist

    Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.
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  8. A18250
    Taltirelin

    TRH-R agonist

    Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).
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  9. A16364
    TC-G-1008

    GPR39 agonist

    TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
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  10. A11625
    Medroxyprogesterone Acetate

    progesterone receptor agonist

    Medroxyprogesterone acetate is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
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  11. A11018
    TAK-875 (Fasiglifam)

    GPR agonist

    TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.
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  12. A12311
    MK-6913

    Estrogen receptor β agonist

    Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.
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  13. A12462
    GPR35 agonist 1

    GPR35/CXCR8 agonist

    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
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  14. A12634
    MBX-2982

    GPR119 agonist

    MBX-2982 is a potential first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion.
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  15. A12982
    MK-6892

    GPR109A agonist

    MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A.K i and GTPγS EC 50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
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  16. A12994
    TUG-770

    FFA1/GPR40 Agonist

    TUG-770 is a Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
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  17. A13193
    SR1001

    ROR agonist

    SR1001 is a selective ROR-alpha and ROR-gamma inverse agonist; suppresses TH17 cell differentiation and inhibits autoimmunity.
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  18. A13248
    MGL-3196

    thyroid hormone receptor agonist

    MGL-3196 is an orally small-molecule liver-directed thyroid hormone receptor agonist designed to increase cholesterol uptake into the liver and increase its metabolism.
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  19. A13249
    AZD5423

    nonsteroidal glucocorticoid receptor agonist

    AZD5423 is a novel nonsteroidal glucocorticoid receptor agonist.
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  20. A13329
    Propyl pyrazole triol

    ERα agonist

    Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist.
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  21. A11431
    Glucocorticoid receptor agonist

    Glucocorticoid receptor agonist

    Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
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  22. A11818
    Avobenzone

    estrogen agonist

    Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
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  23. A12181
    LY2922470

    FFAR1/GPR40 agonist

    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively.

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  24. A13468
    AMG 837 calcium hydrate

    GPR40/FFA1 agonist

    AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.
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  25. A13536
    AEZS-108

    GnRH-1 agonist

    AEZS-108 is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity.
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  26. A13568
    SR-2211

    RORr agonist

    SR-2211 selectively binds RORr(Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORr activity (IC50 = 320 nM).
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  27. A13716
    AR-231453

    GPR119 agonist

    AR-231453 is a potent and selective small molecule agonis of GPR119 that enhances glucose dependent insulin secretion and glucagon like peptide-1 (GLP-1) release.
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  28. A14342
    APD668

    GPR119 agonist

    APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.
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  29. A14542
    GSK137647A

    FFA4/GPR120 agonist

    GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.
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  30. A17038
    TM N1324

    GPR39 agonist

    TM N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
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  31. A17080
    Dexamethasone Phosphate disodium

    glucocorticoid receptor agonist

    Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone.
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  32. A17254
    Beclometasone dipropionate

    glucocorticoid agonist

    Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone.
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  33. A17574
    Canrenone

    Na/K ATPase partial agonist

    Canrenone is a metabolite of spironolactone, Na/K ATPase partial agonist and aldosterone and androgen receptor antagonist used as a diuretic.
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  34. A17986
    Leuprorelin Acetate

    GnRH/LHRH receptor agonist

    Leuprorelin is a Gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, LHRH) receptor agonist. Suppresses estradiol, LH and FSH serum levels and represses the growth of experimental rat endometriosis.
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  35. A17992
    Nafarelin Acetate

    GnRH agonist

    Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH.
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  36. A18177
    Beclometasone

    glucocorticoid receptor agonist

    Beclometasone, also known as Beclomethasone, is an anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma.
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  37. A18236
    Buserelin Acetate

    gonadotropin-releasing hormone agonist

    Buserelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).
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  38. A18335
    TUG-891

    FFA4/GPR120 agonist

    TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism.
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  39. A18343
    GW-870086

    Glucocorticoid receptor agonist

    GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
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  40. A18437
    XY101

    RORγ inverse agonist

    XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
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  41. A18453
    Dexamethasone palmitate

    glucocorticoid receptor agonist

    Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent.
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  42. A20519
    GSK682753A

    EBI2 inverse agonist

    GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
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  43. A20748
    MB-07344

    TR-β agonist

    MB-07344 is a thyroid hormone receptor (TR)-β agonist with a binding affinity Ki of 2.17 nM.
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  44. A20771
    ERB-196

    ERβ agonist

    ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
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  45. A20780
    GNE-6468

    RORγ(RORc) agonists

    GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC50 value of 13 nM for HEK-293 cell.
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  46. A20782
    GNE-0946

    RORγ( RORc) agonist

    GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
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  47. A20796
    Setogepram sodium salt

    GPR40 agonist

    Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84.
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  48. A20902
    PSN632408

    GPR119 receptors agonist

    PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.
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  49. A20968
    Alarelin Acetate

    synthetic GnRH agonist

    Alarelin acetate is a synthetic GnRH agonist.
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  50. A20997
    AVE 0991

    angiotensin-(1-7) receptor agonist

    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
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